Application of cyclodextrin in preparing radioactive iodine labeling hypericum monogynum medicine preparation

A pharmaceutical preparation and radioactive iodine technology are applied in the application field of cyclodextrin in the preparation of radioactive iodine-labeled hypericum drug preparations, can solve the problems of not obtaining and the like, and achieve the advantages of low cost, guaranteed labeling efficiency and fast blood removal. Effect

Inactive Publication Date: 2017-11-03
南京成至诚医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Chinese patent CN201310111593.4 uses cholate to solubilize radioactive iodine-labeled Hypericum drugs, but cholate is used as an adjuvant drug for intravenous injection and has not yet obtained relevant adjuvant approval documents

Method used

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  • Application of cyclodextrin in preparing radioactive iodine labeling hypericum monogynum medicine preparation
  • Application of cyclodextrin in preparing radioactive iodine labeling hypericum monogynum medicine preparation
  • Application of cyclodextrin in preparing radioactive iodine labeling hypericum monogynum medicine preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Traditional formulations (DMSO- 131 I-Hyp is diluted with equal proportions of PEG and propylene glycol) drug preparation:

[0031] First weigh 0.01-13mg Hyp (optimally 1mg), add 1mL DMSO in proportion to obtain 0.01-13mg / mL DMSO-Hyp solution drug (optimally 1mg / mL). Apply the catalyst Iodogen to a 1.5mL EP tube in advance (the optimal ratio is 3-10ug Iodogen:1mCi Na 131 1), add about 1 mL of DMSO-Hyp solution, then add about 1-100 μL of Na 131 I solution (specific activity is 20-1000mCi / mL, the isotope does not exceed 1 half-life from production to use, and the best is 100μL during treatment), vortex and mix continuously and detect the labeling rate until the labeling rate reaches more than 98%, and then Dilute with 1mL PEG and 1mL propylene glycol to obtain DMSO- 131 PEG, propylene glycol diluent of I-Hyp.

[0032] Improved formulation 1 (cyclodextrin- 131 I-Hyp solution) drug preparation:

[0033] First, weigh 0.01-1mg Hyp, add 1mL of 50% hydroxypropyl-β-cyclod...

Embodiment 2

[0037] Contrastive experiment of labeling rate of traditional preparation and improved preparation

[0038] The traditional formulation, improved formulation 1, and improved formulation 2 described in Example 1 were compared for the labeling rate within 7 days; the specific operations were: 0.01-13 mg / mL DMSO-Hyp solution, 0.01 mg / mL cyclodextrin-Hyp solution solution to cyclodextrin-saturated Hyp solution, 0.01-10 mg / mL DMSO-Hyp solution was added with Na 131 I solution, after mixing for a period of time under catalyst Iodogen, adopt thin-layer chromatography (Thin-layer chromatography, TLC), cooperate with gamma counter to detect the concentration of solution 131 I labelling rate.

[0039] Then 0.01-13 mg / mL DMSO- 131 I-Hyp solution is diluted with equal volume of PEG and propylene glycol to obtain traditional preparation; 0.01-10mg / mL DMSO- 131 I-Hyp is diluted with at least 15 times the 50% mass and volume fraction of hydroxypropyl-β-cyclodextrin solution to obtain impr...

Embodiment 3

[0042] Traditional formulation and improved formulation 1 and improved formulation 2 were used in rat experiments 131 I-Hyp biodistribution and necrosis targeting comparative experiment

[0043] Model building:

[0044] Male SD rats (250-300 g) were given 0.5% KI solution instead of drinking water 24 hours before surgery to block the thyroid uptake of free iodine. On the day of the operation, anesthesia and laparotomy were performed, and a right hepatic lobe necrosis and reperfusion operation was performed. Magnetic resonance scanning was performed within 24 hours to detect whether the local liver was necrotic.

[0045] Eighteen hepatic necrosis-reperfusion model rats were selected and randomly divided into 3 groups, 6 rats / group.

[0046] According to the best (optimal) concentration of Example 1, the traditional preparation, the improved preparation 1, and the improved preparation 2 were prepared, and about 100 μCi of various preparations (Hyp dose of 0.1 mg / Kg) were injec...

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Abstract

The invention belongs to the field of medicine preparations, and in particular relates to application of cyclodextrin in preparing a radioactive iodine labeling hypericum monogynum medicine preparation. The cyclodextrin is applied to preparation of a radioactive iodine labeling hypericum monogynum medicine' preparation first a first time; the cyclodextrin is an oligo ring compound of glucose, is non-toxic to human bodies, hydroxypropyl-beta-cyclodextrin is approved by China as an auxiliary material for intravenous injection; meanwhile, compared with other solvents, the auxiliary material can greatly improve the water solubility of hypericin on premise that the iodine labeling efficiency is ensured, the radioactive iodine labeling hypericum monogynum medicine dissolved in the cyclodextrin is rapid in blood clearance, and the necrosis targeting of the medicine is not different from that of conventional preparations, so that the cyclodextrin can be used as a DMSO (Dimethyl Sulfoxide) substituent applied to the radioactive iodine labeling hypericum monogynum medicine preparation; the method for preparing the radioactive iodine labeling hypericum monogynum medicine preparation is simple in process, low in cost, high in preparation efficiency and applicable to industrial operation.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to the application of cyclodextrin in the preparation of radioactive iodine-labeled hypericum pharmaceutical preparations. Background technique [0002] Hypericin (Hyp for short) is an active ingredient extracted from Hypericum perforatum. It can be used for antidepressant treatment, and it is reported to have anti-enveloped virus effect. It has anti-AIDS, hepatitis B and C, simple Herpes virus, chickenpox virus, influenza and other viral infections have a therapeutic effect. In addition, studies have shown that hypericin has no genotoxicity and systemic toxicity to the human body, and is an anti-tumor drug with less toxic and side effects. Hypericin has necrosis affinity, and 80% of solid tumors have spontaneous necrosis inside, so it can be 131 I-labeled hypericin ( 131 I-Hyp) for targeted internal irradiation of tumor necrosis. Nuclide 131 I can emit short-range hi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/40A61K31/122A61K9/08A61K51/06A61P35/00A61K101/02
CPCA61K9/0019A61K9/08A61K31/122A61K47/40A61K51/06
Inventor 倪以政李玥朱孝云张健孙自平蒋维平
Owner 南京成至诚医药科技有限公司
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